Design, synthesis, and antibacterial activities of neomycin-lipid conjugates: Polycationic lipids with potent gram-positive activity
Design, synthesis, and antibacterial activities of neomycin-lipid conjugates: Polycationic lipids with potent gram-positive activity
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DOI：
10.1021/jm800345u
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发表时间：
2008-10-09
影响因子：
7.3
通讯作者：
Schweizer, Frank
中科院分区：
文献类型：
--
作者：
Bera, Smritilekha;Zhanel, George G.;Schweizer, Frank
氨基糖苷类抗生素和阳离子去污剂构成两类临床上重要的药物和防腐剂。然而，由于抗生素耐药性，它们的细菌学和临床疗效最近有所下降。我们已经合成了氨基糖苷类-脂质缀合物，其中氨基糖苷类新霉素形成聚阳离子洗涤剂的阳离子头基。我们的研究结果表明，新霉素-C-16和新霉素-C-20缀合物表现出较强的革兰氏阳性活性，但降低革兰氏阴性活性。新霉素-C-16（C-20）偶联物对耐甲氧西林金黄色葡萄球菌（MRSA）的MIC与临床使用的防腐剂相当。
Aminoglycoside antibiotics and cationic detergents constitute two classes of clinically important drugs and antiseptics. Their bacteriological and clinical efficacy, however, has decreased recently due to antibiotic resistance. We have synthesized aminoglycoside-lipid conjugates in which the aminoglycoside neomycin forms the cationic headgroup of a polycationic detergent. Our results show that neomycin-C-16 and neomycin-C-20 conjugates exhibit strong Gram-positive activity but reduced Gram-negative activity. The MIC of neomycin-C-16 (C-20) conjugates against methicillin-resistant Staphylococcus aureus (MRSA) is comparable to clinically used antiseptics.